Results 221 to 230 of about 37,458 (256)

Profiling Allosteric Modulators of CB ₁ R with an Allosteric Fluoroprobe

Angewandte Chemie
Abstract Allosteric modulation of cannabinoid receptor type 1 (CB 1 R) offers a promising alternative to conventional therapeutic approaches using orthosteric ligands (OLs).
Miroslav Kosar, Themiya Perera, Rudolf L. Z. Ganzoni, Roman C. Sarott, Leire Borrega‐Roman, Rosa Maria Vitale, Alessia Ligresti, Arne C. Rufer, Wolfgang Guba, Uwe Grether, Erick M. Carreira, Dmitry B. Veprintsev, David A. Sykes   +12 more
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The concept of allosteric modulation: an overview

Drug Discovery Today: Technologies, 2013
A brief historical overview of the concept of allosteric interaction is presented together with the different kinds of allosteric control recognized, in the past decades, with the model system of pentameric ligandgated ion channels. Multiple levels of allosteric modulation are identified that include sites distributed in the extracellular ligand ...
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Allosteric modulation of neurotransmission

Biochemical Pharmacology
The therapeutic effects of allosteric modulators on neurotransmission are described. The two unique features of allosteric modulators are: (1) separate binding sites on proteins, and (2) the production of altered receptor conformation upon binding.
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Allosteric Modulation of Dopamine Receptors

Mini-Reviews in Medicinal Chemistry, 2005
Allosteric modulators allow for the fine-tuning of receptor responses to endogenous neurotransmitters and exogenous therapeutic agents. Different types of allosteric modulation of dopamine receptors are discussed as well as the significance of such modulation in the control of normal biological processes and in the treatment of disease.
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Allosteric modulators for the A1 adenosine receptor

Expert Opinion on Therapeutic Patents, 2004
A review. Allosteric modulators of endogenous adenosine represent an alternative to direct acting adenosine agonists and nucleoside uptake blockers. These compds. can selectively enhance the response to adenosine in only those organs or localized areas of a given organ in which prodn. of adenosine is increased. The present article is an overview of the
BARALDI, Pier Giovanni, MOORMAN ALLAN R., AGHAZADEH TABRIZI, Mojgan, PAVANI, Maria Giovanna, ROMAGNOLI, Romeo   +4 more
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Allosteric Adenosine Modulation to Reduce Allodynia

Anesthesiology, 2001
Background Adenosine and adenosine agonists reduce hypersensitivity following inflammation and peripheral nerve injury models of chronic pain. Because inhibitors of adenosine reuptake or metabolism are also effective at reducing hypersensitivity, it is likely that there is a tonic release of spinal adenosine in these models ...
H L, Pan, Z, Xu, E, Leung, J C, Eisenach
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Allosteric Modulation of the Cannabinoid CB1 Receptor

Molecular Pharmacology, 2005
We investigated the pharmacology of three novel compounds, Org 27569 (5-chloro-3-ethyl-1H-indole-2-carboxylic acid [2-(4-piperidin-1-yl-phenyl)-ethyl]-amide), Org 27759 (3-ethyl-5-fluoro-1H-indole-2-carboxylic acid [2-94-dimethylamino-phenyl)-ethyl]-amide), and Org 29647 (5-chloro-3-ethyl-1H-indole-2-carboxylic acid (1-benzyl-pyrrolidin-3-yl)-amide, 2 ...
Martin R, Price, Gemma L, Baillie, Adèle, Thomas, Lesley A, Stevenson, Morag, Easson, Richard, Goodwin, Adèle, McLean, Lorraine, McIntosh, Gillian, Goodwin, Glenn, Walker, Paul, Westwood, Julia, Marrs, Fiona, Thomson, Phillip, Cowley, Arthur, Christopoulos, Roger G, Pertwee, Ruth A, Ross   +16 more
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Allosteric Modulation of Intrinsically Disordered Proteins

2019
The allosteric property of globular proteins is applauded as their intrinsic ability to regulate distant sites, and this property further plays a critical role in a wide variety of cellular regulatory mechanisms. Recent advancements and studies have revealed the manifestation of allostery in intrinsically disordered proteins or regions as allosteric ...
Ashfaq Ur, Rehman, Mueed Ur, Rahman, Taaha, Arshad, Hai-Feng, Chen   +3 more
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Differential Allosteric Modulation of Cas9 Specificity

Journal of Chemical Theory and Computation
Both RNA- and protein-based strategies have been developed to mitigate off-target cleavage by CRISPR-Cas9, yielding noncanonical guide RNAs (gRNAs) and Cas9 variants with enhanced gene-editing precision. However, the molecular mechanisms by which such PAM-distal alterations─remote from the nuclease centers─modulate Cas9 activity and specificity remain ...
Yuanhao Li, Xin Li, Yingjie Chen, Yanqing Wang, Zhicheng Zuo   +4 more
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Allosteric modulators of the extracellular calcium receptor

Drug Discovery Today: Technologies, 2013
The extracellular calcium receptor (CaR) is a Family C G protein-coupled receptor that controls systemic Ca2+ homeostasis, largely by regulating the secretion of parathyroid hormone (PTH). Ligands that activate the CaR have been termed calcimimetics and are classified as either Type I (agonists) or Type II (allosteric activators) and effectively ...
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